CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 µM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor[1][2].
Molekulargewicht:
304.38
Reinheit:
99.64
CAS Nummer:
[1611483-29-4]
Formel:
C18H24O4
Target-Kategorie:
ERK,GABA Receptor
Anwendungsbeschreibung:
MCE Product type: Reference compound
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